公开(公告)号：US11028090B2

公开(公告)日：2021-06-08

申请号：US16480908

申请日：2018-01-25

Applicant: Dong Wha Pharm. Co., Ltd. ,  Korea Research Institute of Chemical Technology

Inventor： Kwangho Lee ,  Gildon Choi ,  Imran Ali ,  Joo Yun Lee ,  Jin Soo Lee ,  Whui Jung Park ,  Yong Tae Kim ,  Seung Hwan Kim ,  Jung Hwan Kim ,  Jae-Kyung Lim

IPC: C07D487/04 ,  A61P35/00 ,  C07D519/00

Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.

公开(公告)号：US10647686B2

公开(公告)日：2020-05-12

申请号：US16347480

申请日：2017-11-01

Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY

Inventor： Kwangho Lee ,  Gildon Choi ,  Na Ri Lee ,  Sang Jun Park ,  Myoung Eun Jung ,  Seong Jin Kim ,  Kyung-Min Yang ,  Jihee Lee

IPC: A61K31/505 ,  C07D239/48 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  C07D405/12

Abstract: The present invention relates to compounds represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is chloro or methyl; R2 is hydrogen or chloro; R3 is hydrogen, fluoro, chloro, bromo, methyl, ethyl, isopropyl, pentyl, hexyl, octyl, methoxy, phenoxy, (4-nitrophenyl)sulfonyl, piperidin-4-yl, or piperazin-1-yl; R4 is hydrogen, chloro, methyl or trifluoromethyl, phenoxy, (4-nitrophenyl)sulfonyl or piperidin-4-yl; or R3 and R4, together with the carbons to which they are attached, form a fused ring selected form the group consisting of: n is 1 or 2. These compounds according to the present invention remarkably inhibits activity of DRAK that inhibits signal systems of TGF-β, which is known to suppress cancer growth, and thus the novel pyrimidine compounds can be used as a pharmaceutical composition for preventing or treating cancer and can be used as a pharmaceutical composition for preventing or treating inflammatory disease.

公开(公告)号：US20200039984A1

公开(公告)日：2020-02-06

申请号：US16480908

申请日：2018-01-25

Applicant: Dong Wha Pharm. Co., Ltd. ,  Korea Research Institute of Chemical Technology

Inventor： Kwangho Lee ,  Gildon Choi ,  Imran Ali ,  Joo Yun Lee ,  Jin Soo Lee ,  Whui Jung Park ,  Yong Tae Kim ,  Seung Hwan Kim ,  Jung Hwan Kim ,  Jae-Kyung Lim

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00

Abstract: Provided are a novel [1,2,4]triazolo[4,3-a]quinoxaline derivative, a method for preparing the same, and a pharmaceutical composition for preventing or treating bromodomain extra-terminal (BET) protein-related diseases including cancer and autoimmune diseases, containing the same as an active ingredient.